CL2A-SN-38 (dichloroacetic acid salt)

CL2A-SN-38 is a cleavable linker-based antibody-drug conjugate (ADC) containing the topoisomerase I inhibitor SN-38 (Cay-15632) and a maleimidocaproyl linker. CL2A-SN-38 has been linked to tumor-selective humanized antibodies, such as anti-Trop-2 (hRS7), to target SN-38 to tumor sites. CL2A-SN-38 linked to hRS7 is cytotoxic to Calu-3, COLO 205, Capan-1, PC3, SK-MES-1, and BxPC-3 cancer cells (IC50s =1.95-23.14 nM). CL2A-SN-38 linked to hRS7 reduces tumor growth in BxPC-3 pancreatic and SK-MES-1 lung cancer mouse xenograft models.Formal Name: carbonic acid, [4-[[(2S)-2-(4-aminobutyl)-35-[4-[[[[4-[(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)methyl]cyclohexyl]carbonyl]amino]methyl]-1H-1,2,3-triazol-1-yl]-1,4,8-trioxo-6,12,15,18,21,24,27,30,33-nonaoxa-3,9-diazapentatriacont-1-yl]amino]phenyl]methyl (4S)-4,11-diethyl-3,4,12,14-tetrahydro-9-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-4-yl ester, dichloroacetic acid. Molecular Formula: C73H97N11O22 . XC2H2Cl2O2. Formula Weight: 1480.6. Purity: >90%. Formulation: (Request formulation change), A solid. Solubility: Methanol: 10 mg/ml. SMILES: O=C1N2C(C(C(C2)=C(C3=C4)CC)=NC3=CC=C4O)=CC5=C1COC([C@@]5(CC)OC(OCC6=CC=C(C=C6)NC([C@H](CCCCN)NC(COCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCN7C=C(N=N7)CNC(C8CCC(CC8)CN9C(C=CC9=O)=O)=O)=O)=O)=O)=O)=O.OC(C(Cl)Cl)=O. InChi Code: InChI=1S/C73H97N11O22.C2H2Cl2O2/c1-3-55-56-39-54(85)16-17-60(56)79-67-57(55)44-83-62(67)40-59-58(70(83)92)46-104-71(93)73(59,4-2)106-72(94)105-45-50-10-14-52(15-11-50)77-69(91)61(7-5-6-20-74)78-64(87)48-103-47-63(86)75-21-23-95-25-27-97-29-31-99-33-35-101-37-38-102-36-34-100-32-30-98-28-26-96-24-22-82-43-53(80-81-82)41-76-68(90)51-12-8-49(9-13-51)42-84-65(88)18-19-66(84)89,3-1(4)2(5)6/h10-11,14-19,39-40,43,49,51,61,85H,3-9,12-13,20-38,41-42,44-48,74H2,1-2H3,(H,75,86)(H,76,90)(H,77,91)(H,78,87),1H,(H,5,6)/t49?,51?,61-,73-,/m0./s1. InChi Key: SNLXRMAUXQVOPQ-RGBFIJSISA-N.